Study of Crystal Structures, Properties, and Form Transformations among a Polymorph, Hydrates, and Solvates of Apatinib
文献类型：期刊论文
| 作者 | Zhu, Bin2; Fang, Xiaoxue2; Zhang, Qi1; Mei, Xuefeng1 ; Ren, Guobin2,3
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| 刊名 | CRYSTAL GROWTH & DESIGN
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| 出版日期 | 2019-05-01 |
| 卷号 | 19期号:5页码:3060-3069 |
| ISSN号 | 1528-7483 |
| DOI | 10.1021/acs.cgd.9b00397 |
| 通讯作者 | Mei, Xuefeng(xuefengmei@simm.ac.cn) ; Ren, Guobin(rgb@ecust.edu.cn) |
| 英文摘要 | Apatinib (APA) is a targeted anti-neoplastic drug by inhibiting the vascular endothelial cell growth factor receptor of tyrosine kinase. Its therapeutic solid form, apatinib mesylate (ATM), is dissociated to APA neutral form instantaneously in aqueous solution. Hereby, we undertook a form screen of APA. A polymorph, two hydrates, and three solvates of APA were discovered and characterized by single-crystal X-ray diffraction, powder X-ray diffraction, Fourier transform infrared, and Raman spectroscopy. The relationships of phase transformation were assessed by differential scanning calorimetry, thermogravimetric analysis, and dynamic vapor sorption. Their thermal and hygroscopic stabilities were elaborated and found to be dependent on intermolecular interaction and crystal packing. Form A with superior solubility and stability appeared to be a promising alternative form to overcome the disproportionation of ATM. |
| WOS关键词 | PHARMACEUTICAL COCRYSTALS ; SOLUBILITY ; SALTS ; STABILITY ; INSIGHT |
| 资助项目 | National Natural Science Foundation of China[21776073] ; National Natural Science Foundation of China[21576080] ; Natural Science Foundation of Shanghai[18ZR1447900] |
| WOS研究方向 | Chemistry ; Crystallography ; Materials Science |
| 语种 | 英语 |
| WOS记录号 | WOS:000466987600063 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/289849]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Mei, Xuefeng; Ren, Guobin |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai 201203, Peoples R China 2.East China Univ Sci & Technol, Sch Pharm, Lab Pharmaceut Crystal Engn & Technol, Shanghai 200237, Peoples R China 3.East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhu, Bin,Fang, Xiaoxue,Zhang, Qi,et al. Study of Crystal Structures, Properties, and Form Transformations among a Polymorph, Hydrates, and Solvates of Apatinib[J]. CRYSTAL GROWTH & DESIGN,2019,19(5):3060-3069. |
| APA | Zhu, Bin,Fang, Xiaoxue,Zhang, Qi,Mei, Xuefeng,&Ren, Guobin.(2019).Study of Crystal Structures, Properties, and Form Transformations among a Polymorph, Hydrates, and Solvates of Apatinib.CRYSTAL GROWTH & DESIGN,19(5),3060-3069. |
| MLA | Zhu, Bin,et al."Study of Crystal Structures, Properties, and Form Transformations among a Polymorph, Hydrates, and Solvates of Apatinib".CRYSTAL GROWTH & DESIGN 19.5(2019):3060-3069. |
入库方式： OAI收割
来源：上海药物研究所
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